title: Synthesis of some novel benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones and studies on the antiproliferative effects and reversal of multidrug resistance of human MDR1-gene transfected mouse lymphoma cells in vitro.
abstract: A new series of benzofuran-2-yl(4,5-diydro-3,5-substituted diphenylpyrazol-1-yl) methanone derivatives 8a-x by the reaction of the benzofuran-2-carbohydrazides 7 with various chalcone derivatives 3a-x using microwave irradiation has been described. The effect of synthesized compounds 8a-v was studied against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells. Among the 24 compounds, the 8c and 8h showed good antiproliferative activity 8b, 8f and 8k were exhibited good MDR reversal activity. The main significance of the process is easy workup process, short reaction time and high yield of the new compounds for biological interest. However, the studies on genetically modified multidrug resistant cancer cells are costly and time consuming.
authors.affiliation: Department of Chemistry, Saurashtra University, Rajkot 360005, India.
authors.forename: Shrey
authors.initials: S
authors.lastname: Parekh
authors.forename: Dhairya
authors.initials: D
authors.lastname: Bhavsar
authors.forename: Mahesh
authors.initials: M
authors.lastname: Savant
authors.forename: Shailesh
authors.initials: S
authors.lastname: Thakrar
authors.forename: Abhay
authors.initials: A
authors.lastname: Bavishi
authors.forename: Manisha
authors.initials: M
authors.lastname: Parmar
authors.forename: Hardevsinh
authors.initials: H
authors.lastname: Vala
authors.forename: Ashish
authors.initials: A
authors.lastname: Radadiya
authors.forename: Nilay
authors.initials: N
authors.lastname: Pandya
authors.forename: Juliana
authors.initials: J
authors.lastname: Serly
authors.forename: Joseph
authors.initials: J
authors.lastname: Molnár
authors.forename: Anamik
authors.initials: A
authors.lastname: Shah
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D016399:Lymphoma, T-Cell / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D008697:Methane / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D015394:Molecular Structure; D021281:Quantitative Structure-Activity Relationship; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D001572:Benzofurans; D008697:Methane